Inhibition of folliculogenesis and ovulation by the antiprogesterone RU 486.
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Treatment with the antiprogesterone RU 486 during the follicular phase of the menstrual cycle inhibited folliculogenesis and ovulation, delaying menses.
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Abstract
Healthy, regularly menstruating women were treated with the antiprogesterone RU 486, Mifepristone (Roussel-Uclaf, Romainville, France) during the follicular phase of the cycle. Three women were given 25 mg of RU 486 on days 1 to 14 of the cycle and five received 25 mg on days 1 to 21 of the cycle. Venous blood samples were collected three times per week during a control cycle and during one treatment cycle in each subject. Serum concentrations of estradiol (E2), progesterone (P), and RU 486 were determined by radioimmunoassays. No drug-related side effects and no spotting or bleeding during RU 486 treatment were observed. Menstrual bleeding was delayed by 8.7 +/- 3.8 days (mean +/- SD) after treatment over days 1 to 14 and by 12.6 +/- 3.2 days after treatment over days 1 to 21. During the treatment with RU 486, the serum concentrations of E2 remained low, indicating effective inhibition of folliculogenesis. After cessation of RU 486 treatment, serum E2 levels rose to similar values as in the control cycle, and subsequently serum P concentrations also reached ovulatory levels in six out of the eight volunteers. The results showed that the antiprogesterone RU 486 delayed folliculogenesis and luteinization even at low doses when given during the follicular phase of the menstrual cycle. It is speculated that this property of RU 486 could be utilized in the design of an estrogen-free combined oral contraceptives.
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References (8)
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Cited by (14)
- Moduladores selectivos del receptor de la progesterona 2016
- Tratamiento de la endometriosis con 5mg o 25mg diarios de mifepristona durante 6 meses. Ensayo clínico aleatorizado, doble ciego 2011
- Safety, tolerability, and pharmacokinetics of a novel, selective antiprogestagen (Org 31710) in healthy male volunteers 1998
- MODERN MEDICAL MANAGEMENT OF ENDOMETRIOSIS 1997
- Inhibition of ovulation by progestin analogs (agonists vs antagonists): Preliminary evidence for different sites and mechanisms of actions 1996
- Pharmacokinetics of mifepristone after low oral doses 1996
- Mifepristone: Clinical Application in General Gynecology 1996
- Progesterone antagonist RU 486 has bone-sparing effects in ovariectomized rats 1995
- Endometrial effects of long-term low-dose administration of RU486 1995
- Dose-Response Relationships of RU 486 1993
- Sequential regimen of the antiprogesterone RU486 and synthetic progestin for contraception 1993
- Mifepristone 1992
- Interruption of endometrial maturation without hormonal changes by an antiprogesterone during the first half of luteal phase of the menstrual cycle: a contraceptive potential 1992
- Endocrine responses to long-term administration of the antiprogesterone RU486 in patients with pelvic endometriosis 1991
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